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RPI-GLYT2-82 | RPI-GLYT2-82 : Non-Competitive/Reversible of SLC6A5
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SLC6A5
    • IC50:554 ± 80 nM
    Non-Competitive/Reversible
    up to 5 uM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    off-target Activity (at 10 μM): DAT -22%, Na channel (site 2) -16%, SERT -88%, NET -1.3%, 5-HT2A -7 ...

    Potency
    Cellular
    In Vitro

    SLC6A5

    Mode of Action: Non-Competitive/Reversible

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.5c03329

    In Vivo Validations

    Mouse
    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 1.49 h
    Systemic clearance: 3844 mL/min/Kg
    Area Under the Curve:: 508.6 h·ng/mL
    Volume of Distribution at Steady-State: 7120 mL/Kg

    DOI Reference: 10.1021/acs.jmedchem.5c03329

    Dose: 50 mg/Kg
    Route of delivery: Oral
    Plasma half life: 0.85 h
    Systemic clearance: 3582.8 h·ng/mL
    Cmax: 2701.6 ng/mL
    Tmax: 0.5 h
    Bioavailability: 27.6%

    DOI Reference: 10.1021/acs.jmedchem.5c03329

    Dose: 30 mg/Kg
    Route of delivery: Intraperitoneal
    Plasma half life: 1.08 ± 0.05 h
    Systemic clearance: 2063.72 ± 313.68 mL/min/Kg
    Cmax: 152 ± 31 ng/mL
    Tmax: 1.0 ± 0 h
    Area Under the Curve:: 241 ± 40 h*ng/mL
    Volume of Distribution at Steady-State: 192.93 ± 23.32 L/Kg

    DOI Reference: 10.1038/s41467-026-69616-5

    Chemical Information

    Coming Soon...

    References

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    Expert Reviews

    No SERP comments found for RPI-GLYT2-82

    Probe RPI-GLYT2-82 is in the process of SERP review.

    Please continue to check back for new reviews and commentary.